Comparison of metabolic ratios of CYP3A5 and its mutants with those of CYP3A4
The enzymes indicated were transiently expressed in COS-7 cells. Metabolism experiments for maraviroc were performed, and oxidative metabolites M1, M2, and M3 were measured as described under Materials and Methods. Metabolic ratios (M1/M2 and M1/M3) are presented as means ± S.D.
| Name | M1/M2 | M1/M3 |
|---|---|---|
| CYP3A5 | 24.4 ± 1.3 | 30.4 ± 4.2 |
| L57F | 11.8 ± 1.2 | 13.6 ± 1.4 |
| S107P | 24.1 ± 2.7 | 10.9 ± 4.0 |
| L108F | 1.29 ± 0.05 | 1.7 ± 0.03 |
| F146V | 20.0 ± 2.9 | 25.6 ± 4.0 |
| G186S | 25.4 ± 1.5 | 38.9 ± 3.2 |
| S206N | 34.0 ± 2.1 | 47.6 ± 3.6 |
| G214D | 6.14 ± 0.2 | 4.6 ± 0.03 |
| L219F | 17.9 ± 0.4 | 16.7 ± 0.1 |
| S239C | 27.3 ± 4.0 | 42.3 ± 3.9 |
| L240V | 13.3 ± 6.3 | 14.9 ± 4.9 |
| V369I | 18.2 ± 4.5 | 25.1 ± 2.8 |
| I371M | 20.3 ± 2.8 | 15.0 ± 1.5 |
| S392V | 22.5 ± 0.1 | 18.8 ± 2.3 |
| T478L | 25.6 ± 2.7 | 38.1 ± 2.7 |
| Q479G | 25.6 ± 2.2 | 23.4 ± 1.1 |
| CYP3A4 | 1.5 ± 0.5 | 1.6 ± 0.8 |